TRK II-IN-1,2904690-41-9

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TRK II-IN-1

CAS No. : 2904690-41-9

MCE 国际站：TRK II-IN-1

产品活性：TRK II-IN-1 是一种有效的 II 型 TRK 抑制剂，抑制 TRKA/B/C and TRKA^G667C 的 IC₅₀ 值分别为3.3，6.4，4.3 和 9.4 nM。TRK II-IN-1还可以抑制 FLT3，RET 和 VEGFR2，IC₅₀ 值分别为 1.3，9.9 和 71.1 nM。TRK II-IN-1 可用于研究 TRK 驱动的癌症。

研究领域：Neuronal Signaling  |  Protein Tyrosine Kinase/RTK

作用靶点：Trk Receptor  |  FLT3  |  VEGFR  |  RET

In Vitro: TRK II-IN-1 (compound 12d) (1 μM) demonstrates over 90% of kinase inhibition towards VEGFR2, RET, FLT3 and nearly 70% inhibition against Kit, CSF1R, DDR1 and DDR2.
TRK II-IN-1 (72 h) inhibits Ba/F3-CD74-TRKA, Ba/F3-ETV6-TRKB and Ba/F3-ETV6-TRKC cells, with IC₅₀s of 26.1, 44.7 and 15.7 nM, respectively.
TRK II-IN-1 (72 h) suppresses proliferation of a panel of Ba/F3 cells stably transformed with wild type, xDFG as well as solvent-front (SF) mutant TRK fusion proteins, with IC₅₀s ranging from 2.6 to 143.3 nM.
TRK II-IN-1 (0.4-500 nM; 48 h) induces apoptosis of Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKA^G667C cells.
TRK II-IN-1 (0.4-500 nM; 24 h) arrests cell cycle progression in the G0/G1 phase in Ba/F3-CD74-TRKA and Ba/F3-CD74-TRKA^G667C cells.
TRK II-IN-1 (0.8-500 nM; 6 h) suppresses the phosphorylation of TRKA, TRKA^G667C kinases, and their downstream AKT, ERK and PLCγ1 in a dose-dependent manner.

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